title: Novastan (brand of argatroban): a small-molecule, direct thrombin inhibitor.
abstract: Because of the unsatisfactory options available for safe and effective antithrombotic therapy, recent, intense research and development efforts have focused on direct, or site-directed, thrombin inhibitors. Argatroban is a small-molecule, reversible, direct thrombin inhibitor selective for the catalytic site of the thrombin molecule. Argatroban's molecular properties (small molecule; fast, selective, and reversible inhibition of the thrombin catalytic site; and similar in vitro potency for inhibiting both clot-bound and soluble thrombin) offer the potential for significant antithrombotic efficacy with minimal systemic anticoagulant effects. Its clinical pharmacologic properties offer the potential for minimal risk of bleeding, very rapid achievement of therapeutic antithrombotic efficacy, predictable dose response, and rapid restoration of the hemostatic systems to baseline on termination of intravenous infusion. The intravenous agent Novastan (brand of argatroban) is currently approved for clinical use in Japan for the treatment of peripheral arterial occlusive disease. Novastan is in advanced clinical development in North and South America for several indications, including (1) anticoagulant/antithrombotic therapy in heparin-induced thrombocytopenia (HIT) and heparin-induced thrombocytopenia, and thrombosis syndrome (HITTS); and (2) adjunctive therapy to thrombolytic agents in acute myocardial infarction. Results from these trials are projected to be available by early 1997.
authors.affiliation: Texas Biotechnology Corporation, Houston 77030, USA.
authors.forename: M J
authors.initials: MJ
authors.lastname: Hursting
authors.forename: K L
authors.initials: KL
authors.lastname: Alford
authors.forename: J C
authors.initials: JC
authors.lastname: Becker
authors.forename: R L
authors.initials: RL
authors.lastname: Brooks
authors.forename: J L
authors.initials: JL
authors.lastname: Joffrion
authors.forename: G D
authors.initials: GD
authors.lastname: Knappenberger
authors.forename: P W
authors.initials: PW
authors.lastname: Kogan
authors.forename: T P
authors.initials: TP
authors.lastname: Kogan
authors.forename: A A
authors.initials: AA
authors.lastname: McKinney
authors.forename: R P
authors.initials: RP
authors.lastname: Schwarz
mesh_terms: D000818:Animals; D000991:Antithrombins / Q000627:therapeutic use*; D001120:Arginine / Q000031:analogs & derivatives; D017321:Clinical Trials, Phase I as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D015394:Molecular Structure; D008970:Molecular Weight; D009203:Myocardial Infarction / Q000628:therapy; D010875:Pipecolic Acids / Q000627:therapeutic use*; D013449:Sulfonamides; D015912:Thrombolytic Therapy
chemical_list: D000991:Antithrombins; D010875:Pipecolic Acids; D013449:Sulfonamides; D001120:Arginine; C031942:argatroban